SHU 9119
Based on 3 publication(s) in Google Scholar
SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
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- Pureté: 99.83%
- CAS No.: 168482-23-3
- Formule: C54H71N15O9
- Masse moléculaire:1074.24
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Stockage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications Citing Use of MedChemExpress (MCE) SHU 9119
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Activité biologique
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MC3R |
MC4R |
MC5R |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.67 nM
Compound: SHU9119
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Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
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[PMID: 25699138] |
| HEK293 | EC50 |
2.4 nM
Compound: SHU9119
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Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
|
[PMID: 25699138] |
| HEK293 | EC50 |
3 nM
Compound: SHU9119
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Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
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[PMID: 25699138] |
| HEK293 | EC50 |
>100000 nM
Compound: SHU9119
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Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
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[PMID: 25699138] |
| HEK293 | EC50 |
0.64 nM
Compound: SHU9119
|
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
|
[PMID: 25898270] |
| HEK293 | EC50 |
2.31 nM
Compound: SHU9119
|
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay
|
[PMID: 25898270] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 168482-23-3
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Appearance Solid
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Masse moléculaire 1074.24
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Formule C54H71N15O9
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Color White to off-white
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Sequence
Ac-{Nle}-Asp-His-{d-Nal}-Arg-Trp-Lys-NH2 (Lactam bridge: Asp2-Lys7)
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Sequence Shortening
Ac-{Nle}-DH-{d-Nal}-RWK-NH2 (Lactam bridge: Asp2-Lys7)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Paraventricular hypothalamic RUVBL2 neurons suppress appetite by enhancing excitatory synaptic transmission in distinct neurocircuits. [Abstract]2024 Oct 16;15(1):8939. PMID: 39414808 -
Sci Adv
27-Hydroxycholesterol acts on estrogen receptor α expressed by POMC neurons in the arcuate nucleus to modulate feeding behavior. [Abstract]2024 Jul 12;10(28):eadi4746. PMID: 38996023 -
Gene
Effects and regulatory pathway of proopinmelanocortin on feeding habit domestication in mandarin fish. [Abstract]2023 Aug 20:878:147581. PMID: 37336270
Solvant et solubilité
H2O : 10 mg/mL (9.31 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
Rats: SHU9119 is prepared in saline. SHU9119 is infused i.c.v. at a concentration of 24 nM and MTII at a concentration of 1 nM per day for 2 or 7 days. To differentiate between SHU9119 effects per se from those related to increased food intake, we prevent overeating in a group of SHU9119-treated rats by pair-feeding, so that they are given the same amount of food as consumed by a control group (SHU9119-pf). The pair-feeding regimen consists in giving one-third of the daily food amount in the morning and the remaining two-thirds just before onset of darkness. Thus, most of the experiments include 5 groups of animals: an ad libitum–fed control group infused with i.c.v. saline; 2 i.c.v. SHU9119-infused groups: SHU9119–ad lib and SHU9119-pf; an MTII-infused group; and a saline-pf group[2].
Mice: SHU9119 is prepared in artificial cerebrospinal fluid. After 4 weeks of run-in diet, mice are randomized into groups that received icv administration of artificial cerebrospinal fluid (vehicle) or SHU9119 (5 nmol/day) in vehicle during 14-17 days. The effect of SHU9119 on BAT activity independent of food intake is also investigated by using an additional SHU9119-treated group that is pair-fed (SHU9119-pf) to the vehicle-treated group. To achieve pair-feeding, food intake of the ad libitum-fed mice is monitored daily, and pair-fed mice receive surgery 1 day behind the control mice. The pair-feeding regimen consisted of giving the mice the average daily consumed food amount by the control mice, just before onset of darkness[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Grieco P, et al. Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. Peptides. 2007 Jun;28(6):1191-6. [Content Brief]
[2]. Nogueiras R, et al. The central melanocortin system directly controls peripheral lipid metabolism. J Clin Invest. 2007 Nov;117(11):3475-88. [Content Brief]
[3]. Kooijman S, et al. Inhibition of the central melanocortin system decreases brown adipose tissue activity. J Lipid Res. 2014 Oct;55(10):2022-32. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.9309 mL | 4.6545 mL | 9.3089 mL | 23.2723 mL |
| 5 mM | 0.1862 mL | 0.9309 mL | 1.8618 mL | 4.6545 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.